| 摘要 |
Heterocyclic guanidines and isothioureas of formula: Het-(CH2)3-NH.C(=N.Y).W-(CH2)q-W-C(=X)-NH(CH2)nZ(CH2)m-Het' (I) and their addition salts with pharmaceutically acceptable acids are new: In the formula Het = pyridyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, thiadiazolyl, pyrimidyl, pyrazinyl or pyridazinyl, opt. subst. by halo, lower alkyl or alkoxy, OH or NH2, Y = H, OH or lower alkyl, X = S, CHNO2 or NY', Y' = H, OH, lower alkyl, CN or CONH2, W = NH or equally, when NY and X are both NH, also S, q = 2-12, n = 2-3, m = 0-2, provided that m+n = 3-4, or m+n can also be 2 when X is NH, NOH, NCONH2 or N alkyl and Het' = imidazolyl, pyrazolyl or triazolyl. Z = S or CH2, Het' = 5-6 membered N-heterocycle e.g. as defined for Het, imidazolyl, triazolyl or pyrazolyl, opt. substd. as for Het. Pref. cpds. have W = X=NH Y = H and q=6-10. (I) block the H2 histamine receptors which are not blocked by conventional antihistamines such as mepyramine. They are thus useful as antisecretories, antiphlogistics and cardiovascular agents. The usual daily dose is 0.15-1.5g. |
